Asthma

Question 1

Name 8 Beta-2 agonists. Which are short-acting and which are long acting?

Answer 1

Short acting:
Albuterol, Levalbuterol, terbutaline, metopreterenol, pirbutol
Long acting:
Salmeterol, Formoterol, Indacaterol (only COPD)

Question 2

What are the adverse effects of Terbutaline and others in its class?

Answer 2

(beta-2 agonist)
-selectivity is lost with high doses- beta-1 effects:
tremor, tachycardia, tolerance, etc.

Question 3

Salmeterol and others in its class must be used in combination with what other class of drug?

Answer 3

(long acting beta-2 agonist)

must be used with inhaled corticosteriods (increase transcription of beta-2 receptor)

Question 4

What are 3 anti-muscarinic agents used in the treatment of asthma? Mechanism of action?

Answer 4

Ipratropium
Tiotropium
Atropine
–> inhibition of mainly M3 receptors; Block vagal pathways and decreases vagal tone to bronchial smooth muscle; also blocks the reflex bronchoconstriction caused by inhaled irritants

Question 5

Which anti-muscarinic agent has the longest half-life at the M3 receptor? Beside bronchodilation, what other effects does it have?

Answer 5

Tiotropium (M3 half-life 34hrs)

–> anti-inflammatory; decreases mucus production

Question 6

What is Aclidinium bromide?

Answer 6

• similar to Tiotropium with greater M3 affinity and half life at M3 29hrs
• rapidly metabolized in plasma so less systemic and CNS side effect and higher doses can be given safely

Question 7

What is first line treatment for chronic stable COPD?

Answer 7

Tiotropium

Question 8

What are 3 Methylxanthines? Mechanism of action (3)?

Answer 8

Theophylline, Theobromine, Caffeine

1. non-selective PDE inhibitors –> bronchdilation
2. histone deacetylation –> suppress inflammatory genes
3. improve contractility and reverse fatigue of diaphragm in COPD

Question 9

What is Roflumilast?

Answer 9

Selective PDE4 inhibitor

–>anti-inflammatory- inhibits neutrophil migration (may be used for COPD)

Question 10

What class of drugs is used as prophylaxis for exercise induced bronchospasm and the drug of choice for aspirin induced asthma?

Answer 10

Leukotriene Inhibitors (montelukast, pranlukast, zafirlukast)
[only effective for mild cases]

Question 11

What is the mechanism of action and use of Sodium cromoglycate & Nedocromil sodium?

Answer 11

• prevents mast cell degranulation and mediator release from macrophage and eosinophil
• weak, used in pediatrics as preventive treatment before exercise or exposure to allergens

Question 12

What is Omalizumab? Use?

Answer 12

Anti-IgE monoclonal antibody
–> subQ injection every 2-4 weeks
reduces asthma exacerbations
used only in patients with poorly controlled severe asthma

Question 13

What is the treatment for acute asthma exacerbation and COPD?

Answer 13

-systemic corticosteroids (5-7days)
-short-acting beta-2 agonist
-short-acting anticholinergic via nebulizer
-Abx for COPD exacerbation
[no role for long-acting drugs]